Design, synthesis, and apoptotic antiproliferative activity of novel dihydropyrimidine-5-carbonitrile/1,2,4-oxadiazole hybrids as dual EGFR/VEGFR-2 inhibitors endowed with antioxidant activity.

ABSTRACT: A new series of dihydropyrimidine-5-carbonitrile/1,2,4-oxadiazole hybrids (10a-l) was developed as dual inhibitors of EGFR and VEGFR-2. The structures of the newly synthesized compounds were confirmed using ¹H NMR, ¹³C NMR, and elemental analysis. The novel compounds were evaluated for their antioxidant and antiproliferative apoptotic characteristics. Compounds 10e, 10k, and 10l demonstrated the most potent antiproliferative activity and exhibited more efficacy than the reference erlotinib against both Panc-1 (pancreatic) and MCF-7 (breast) cancer cell lines. Compounds 10k and 10l exhibited the highest potency as EGFR and VEGFR-2 inhibitors, with IC₅₀ values of 57 nM and 61 nM against EGFR, respectively, and IC₅₀ values of 21 nM and 26 nM for VEG

SUBMITTER: Al-Wahaibi LH 

PROVIDER: S-EPMC12530851 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature